The metabolism and disposition of [ 14 C]apixaban, an orally bioavailable, highly selective,
and direct acting/reversible factor Xa inhibitor, was investigated in 10 healthy male subjects …

The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor
which reduced blood glucose levels in a dose-dependent manner by as much as 55% in …

Several human immunodeficiency virus (HIV) protease inhibitors, including atazanavir,
indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir, were tested for their potential to inhibit …

An improved mass defect filter (MDF) method employing both drug and core structure filter
templates was applied to the processing of high resolution liquid chromatography/mass …

Mass spectrometry plays a key role in drug metabolite identification, an integral part of drug
discovery and development. The development of high-resolution (HR) MS instrumentation …

SPRYCEL (dasatinib, BMS-354825; Bristol-Myers Squibb, Princeton, NJ), a multiple kinase
inhibitor, is currently approved to treat chronic myelogenous leukemia and Philadelphia …

(2S,3R,4R,5S,6R)-2-(3-(4-Ethoxybenzyl)-4-chlorophenyl)-6-hydroxymethyl-tetrahydro-2H-pyran-3,4,5-triol
(dapagliflozin; BMS-512148) is a potent sodium-glucose cotransporter type II …

High throughput screening identified 2-acetamido-thiazolylthio acetic ester 1 as an inhibitor
of cyclin-dependent kinase 2 (CDK2). Because this compound is inactive in cells and …

A sensitive and quantitative method was developed for the estimation of reactive metabolite
formation in vitro. The method utilizes reduced glutathione (GSH) labeled with a …

In most cases, the metabolism of drugs leads to pharmacological inactivation through
biotransformation to therapeutically inactive molecules. However, drug metabolism can also result …